Literature DB >> 6140061

Characterization of the opiate receptor population mediating inhibition of VIP-induced secretion from the small intestine of the rat.

I M Coupar.   

Abstract

Net water transport was measured from the jejunum of anaesthetized rats by a re-circulation technique. Several narcotic analgesics were administered intravenously and assessed for activity in reversing net fluid secretion induced by intra-arterial infusion of vasoactive intestinal peptide (VIP). The mu-opiate agonists, morphine, RX 783006 and FK 33-824 produced full reversal of the secretory phase of the VIP response, but failed to restore totally fluid transport to the control level of net absorption. The kappa-agonist, ethylketocyclazocine, caused only partial reversal of VIP-induced secretion while the more selective kappa-agonist, MR 2034, produced a small though non-significant antisecretory effect at high doses. The delta-agonist, D-Ala2-D-Leu5-enkephalin also had negligible antisecretory activity. Naloxone caused a parallel displacement to the right of the antisecretory dose-response line to morphine. The 'in vivo pA2' value of naloxone was 7.14. The results are compared with previously published antinociceptive activities of the opiate agonists and in vivo pA2 values of naloxone. It is concluded that stimulation of mu-opiate receptors mediates inhibition of VIP-induced fluid secretion from the rat jejunal mucosa.

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Year:  1983        PMID: 6140061      PMCID: PMC2045039          DOI: 10.1111/j.1476-5381.1983.tb10043.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  26 in total

1.  Studies on the direct spinal action of narcotics in the production of analgesia in the rat.

Authors:  T L Yaksh; T A Rudy
Journal:  J Pharmacol Exp Ther       Date:  1977-08       Impact factor: 4.030

2.  A synthetic enkephalin analogue with prolonged parenteral and oral analgesic activity.

Authors:  D Roemer; H H Buescher; R C Hill; J Pless; W Bauer; F Cardinaux; A Closse; D Hauser; R Huguenin
Journal:  Nature       Date:  1977-08-11       Impact factor: 49.962

3.  Comparison of the behavioral effects of beta-endorphin and enkephalin analogs.

Authors:  E T Wei; L F Tseng; H H Loh; C H Li
Journal:  Life Sci       Date:  1977-08-01       Impact factor: 5.037

4.  The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.

Authors:  W R Martin; C G Eades; J A Thompson; R E Huppler; P E Gilbert
Journal:  J Pharmacol Exp Ther       Date:  1976-06       Impact factor: 4.030

Review 5.  Neurobiology and neuropharmacology of the enkephalins.

Authors:  R J Miller; P Cuatrecasas
Journal:  Adv Biochem Psychopharmacol       Date:  1979

6.  Inhibition of stimulated fluid secretion in the rat small and large intestine by opiate agonists.

Authors:  E Beubler; F Lembeck
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1979-03       Impact factor: 3.000

7.  The relationship between pharmacokinetics and pharmacodynamic action as applied to in vivo pA2: application to the analgesic effect of morphine.

Authors:  R J Tallarida; C Harakal; J Maslow; E B Geller; M W Adler
Journal:  J Pharmacol Exp Ther       Date:  1978-07       Impact factor: 4.030

8.  Quantitative studies on the antagonism by naloxone of some narcotic and narcotic-antagonist analgesics.

Authors:  S E Smits; A E Takemori
Journal:  Br J Pharmacol       Date:  1970-07       Impact factor: 8.739

9.  Inhibition by morphine of prostaglandin-stimulated fluid secretion in rat jejunum.

Authors:  I M Coupar
Journal:  Br J Pharmacol       Date:  1978-05       Impact factor: 8.739

10.  In vivo antagonism by naloxone of morphine, beta-endorphin and a synthetic enkephalin analog.

Authors:  J I Székely; Z Dunai-Kovács; E Miglécz; A Z Rónai; S Bajusz
Journal:  J Pharmacol Exp Ther       Date:  1978-12       Impact factor: 4.030

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  2 in total

1.  Voltage-clamp experiments reveal receptor type-dependent modulation of chloride secretion in the guinea pig colonic mucosa by intestinal opioids.

Authors:  W Kromer
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1991-09       Impact factor: 3.000

2.  Difenoxin and loperamide: studies on possible mechanisms of intestinal antisecretory action.

Authors:  A De Luca; I M Coupar
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1993-02       Impact factor: 3.000

  2 in total

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